Neovascularization plays a role in several pathological conditions, including tumor growth, arthritis, and choroidal neovascularization. Preliminary in vitro Matrigel angiogenesis assays on the EtOH extracts of Chinese herbal medicine revealed that the hexane layer of Lespedeza cuneata was active against the formation of tube-like structures on Matrigel. L. cuneata is a perennial legume distributed in Korea, China, India, Australia and Taiwan and used as folk anti-inflammatory medicine. By anti-angiogenetic activity-guided silica gel chromatography of the hexane layer, a low-polarity fraction containing polyunsaturated fatty acids with IC50 of 8μg/ml was obtained. It had been proved that long chain n-3 polyunsaturated fatty acids have anti-angiogenic effect in intestinal microvascular endothelium. We also isolated and identified 3 triterpenes (LC-3 & 4) among which stigmasterol and ß-sitosterol had been reported to have anti-inflammatory properties along with two other compounds, salicylic acid (LC-1) and (65,7E)-vomifoliol (LC-2).